Palladium-Catalyzed Arylation of Carbasugars Enables the Discovery of Potent and Selective SGLT2 Inhibitors
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AbstractSelective inhibition of the transporter protein sodium-glucose cotransporter 2 (SGLT2) has emerged as a promising way to control blood glucose level in diabetes patients. Reported herein is a short and convergent synthetic route towards some small-molecule SGLT2 inhibitors by a chemo-and diastereospecific palladium-catalyzed arylation reaction. This synthetic strategy enabled the discovery of two highly selective and potent SGLT2 inhibitors, thereby paving the way towards the development of carbasugar SGLT2 inhibitors as potential antidiabetic/antitumor agents.
All Author(s) ListNg WL, Lau KM, Lau CBS, Shing TKM
Journal nameAngewandte Chemie International Edition
Year2016
Month10
Day1
Volume Number55
Issue Number44
PublisherWILEY-V C H VERLAG GMBH
Pages13818 - 13821
ISSN1433-7851
eISSN1521-3773
LanguagesEnglish-United Kingdom
Keywordscarbohydrates; cross-coupling; drug design; inhibitors; palladium
Web of Science Subject CategoriesChemistry; Chemistry, Multidisciplinary

Last updated on 2020-22-10 at 02:21